Inhibitors of farnesyl-protein transferase

Details Inhibitors of farnesyl-protein transferase Inhibitors of farnesyl-protein transferase

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/47 (2006.01) A61K 38/00 (2006.01) A61P 9/00 (2006.01) A61P 9/10 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01) C07D 401/14 (2006.01) C07D 403/00 (2006.01) C07D 403/12 (2006.01) C07D 409/00 (2006.01) C07D 417/00 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01)

Patent

CA 2216654

The present invention comprises analogs of the CA1A2X motif of the protein Ras that is modified by farnesylation in vivo. These CA1A2X analogs inhibit the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, these CA1A2X analogs differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. The compounds of the instant invention also incorporate a cyclic amine moiety in the A2 position of the motif. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

La présente invention concerne des analogues du motif CA<1>A<2>X de la protéine Ras modifiés par farnesylation in vivo. Ces analogues CA<1>A<2>X ont un effet inhibiteur sur la farnésyl-protéine transférase et sur la farnesylation de certaines protéines. En outre, ces analogues CA<1>A<2>X diffèrent de ceux décrits antérieurement en tant qu'inhibiteurs de farnésyl-protéine transférase par le fait qu'ils ne comportent pas de fraction thiol. L'absence de thiol présente des avantages uniques en termes d'amélioration du comportement pharmacocinétique chez les animaux, de prévention de réactions chimiques dépendantes d'un thiol, telle que l'auto-oxidation rapide et les formations de bisulfure avec des thiols endogènes, et une toxicité systémique réduite. Les composants de cette invention renferment également une fraction amine cyclique à la position A<2> du motif. Cette invention recouvre également des compositions chimiothérapeutiques renfermant de tels inhibiteurs de farnesyl transférase et leurs procédés de production.

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